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ABT-384

Alias: ABT 384 ABT384 ABT-384
Cat No.:V9982 Purity: ≥98%
ABT-384 is a potent and specific 11-beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor.
ABT-384
ABT-384 Chemical Structure CAS No.: 868623-40-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
ABT-384 is a potent and specific 11-beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor. ABT-384 has high affinity for rodent, monkey and human 11β-HSD1, with Kis in the range of 0.1-2.7 nM. ABT-384 blocks the regeneration of active cortisol. ABT-384 could be used in Alzheimer's disease (AD) research.
Biological Activity I Assay Protocols (From Reference)
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H34F3N5O2
Molecular Weight
493.564976215363
Exact Mass
493.266
Elemental Analysis
C, 60.84; H, 6.94; F, 11.55; N, 14.19; O, 6.48
CAS #
868623-40-9
PubChem CID
11670435
Appearance
White to off-white solid powder
LogP
2.6
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
5
Heavy Atom Count
35
Complexity
825
Defined Atom Stereocenter Count
0
InChi Key
CLHMYBJIOZXCEX-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H34F3N5O2/c1-23(2,33-7-5-32(6-8-33)19-4-3-18(14-30-19)25(26,27)28)22(35)31-20-16-9-15-10-17(20)13-24(11-15,12-16)21(29)34/h3-4,14-17,20H,5-13H2,1-2H3,(H2,29,34)(H,31,35)
Chemical Name
4-[[2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanoyl]amino]adamantane-1-carboxamide
Synonyms
ABT 384 ABT384 ABT-384
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~31.25 mg/mL (~63.32 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0261 mL 10.1303 mL 20.2606 mL
5 mM 0.4052 mL 2.0261 mL 4.0521 mL
10 mM 0.2026 mL 1.0130 mL 2.0261 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01009216 Completed Drug: ABT-384 Healthy Abbott 2009-10 Phase 1
NCT00968422 Completed Drug: ABT-384
Drug: Matching placebo to ABT-384
Healthy Abbott 2009-08 Phase 1
NCT01137526 Completed Drug: ABT-384
Drug: donepezil
Drug: placebo
Alzheimer's Disease AbbVie (prior sponsor, Abbott) 2010-05 Phase 2
Biological Data
  • ABT-384 inhibits its target 11-beta-hydroxysteroid dehydrogenase type 1 (HSD-1) in the liver. Spot urine samples were collected before dosing and four times between 2 and 40 h after five daily doses of ABT-384. The HSD-1 ratio is urine cortisol metabolites (5-α-tetrahydrocortisol+5-β-tetrahydrocortisol) divided by urine cortisone metabolite (tetrahydrocortisone). The median of two individuals is represented for each regimen.[1]. Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384. Transl Psychiatry. 2013;3(8):e295. Published 2013 Aug 27.
  • ABT-384 inhibits its target 11-beta-hydroxysteroid dehydrogenase type 1 (HSD-1) in the periphery. Plasma samples were collected hourly during D4 cortisol infusions. D4 cortisol was infused on Day 5 from just after the last dose of ABT-384 for 8 h and again for 8 h starting either 22 (10, 50 mg) or 32 h (1, 2 mg) after the last dose of ABT-384. Subjects who did not receive ABT-384 received only one D4 cortisol infusion. The median of two individuals is represented for each regimen. Upper panels show the ratio (D3 cortisol/D3 cortisone) that is a direct measure of HSD-1 activity. Lower panels show the ratio (D3 cortisol/D4 cortisol) that is a measure of flux through the HSD-2+HSD-1 pathway.[1]. Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384. Transl Psychiatry. 2013;3(8):e295. Published 2013 Aug 27.
  • ABT-384 inhibits its target 11-beta-hydroxysteroid dehydrogenase type 1 (HSD-1) in the central nervous system (CNS). Cerebrospinal fluid (CSF) samples were collected hourly during D4 cortisol infusions. D4 cortisol was infused on Day 5 from just after the last dose of ABT-384 for 8 h and again for 8 h starting either 22 (10, 50 mg) or 32 h (1, 2 mg) after the last dose of ABT-384. Subjects who did not receive ABT-384 received only one D4 cortisol infusion. Results are not presented for hour 2 owing to a sample collection problem in one of these two subjects. The median of two individuals is represented for each regimen. See Discussion for potential explanations of negative intrinsic CSF D3 cortisol values.[1]. Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384. Transl Psychiatry. 2013;3(8):e295. Published 2013 Aug 27.
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